Trends in most common drug targets

This table illustrates the top 20 targets for drugs other than vaccines and advanced biologicals, like CAR T cells. Note, proteins binding with the Fc region of antibodies have been removed from the table. The presence is calculated by the number of trials in which a particular target has been drugged. If a single trial contains more than one agent that targets a particular drug target, this trial is counted as the number of these agents. Max phase column illustrates the maximal phase of a clinical trial in which a particular target has appeared. Trials with phase four have not been included because of the fact they contain agents that were never approved for brain tumors, and likely their phase is not equal for all analyzed treatment arms. Approved drug targets are labeled as approved. The number of clinical trials is calculated by the number of trials in which a particular target has been drugged, and each trial is counted only once, no matter the number of agents against the target. The number of unique drugs illustrates the number of drugs that exploit the target. For each drug, both pivotal and secondary targets were taken into account. The trend was calculated as follows: if a 3-year avg. of the target presence during 2017, 2018, and 2019 is 10% or more higher than the avg. during the 10-year period, the trend is upward, whereas if it is 10% or more below than the avg. during the 10-year period, the trend is downward. The year column illustrates the first year the target appeared during the analyzed 10 years of brain cancer trials. Data are to February 2020.

TargetPresenceMax. PhaseNumber of Trials with TargetNumber of Unique Agents Drugging the TargetTrendEarliest Year
DNA422Approved37027No trend2010
VEGFA109Approved1083Downward trend2010
PDCD1783787Upward trend2013
NR1I26436214No trend2010
KDR6025719No trend2010
PTGS2593549No trend2010
PPARG523516Upward trend2010
EGFR5024925No trend2010
MTOR48Approved4714Downward trend2010
PTGS1463465Upward trend2010
TUBB14634516Downward trend2010
ACAT1453454Upward trend2010
FLT14524513No trend2010
KIT4524213Downward trend2010
PDGFRB4223911Downward trend2010
FLT44124112Downward trend2010
HRH2403402Upward trend2010
TOP1362367Downward trend2010
PDGFRA3423312Downward trend2010
TOP1MT332334Downward trend2010
TOP2A3232911Downward trend2010
HDAC22832810Downward trend2010
FGFR12622510Downward trend2010
TACSTD2262264Downward trend2010
TYMS262237Downward trend2010

DNA, deoxyribonucleic acid; EGFR, epidermal growth factor receptor; FGFR1, fibroblast Growth Factor Receptor 1; FLT1, vascular endothelial growth factor receptor 1; FLT4, fms-related tyrosine kinase 4; HDAC2, histone Deacetylase 2; KDR, kinase insert domain recepto; KIT, protooncogene c-KIT; MTOR, mechanistic target of rapamycin; NR1I2, nuclear Receptor subfamily 1, group I, member 2; PDCD1, Programmed cell death protein 1; PDGFRA, platelet-derived growth factor receptor A; PDGFRB, plateletderived growth factor receptor beta; TACSTD2, tumor associated calcium signal transducer 2; TOP1, DNA topoisomerase 1; TOP1MT, DNA Topoisomerase I Mitochondrial; TOP2A, DNA Topoisomerase II Alpha; TUBB1, tubulin beta-1 chain; TYMS, thymidylate synthetase; VEGFA, vascular endothelial growth factor A.